Yoshikawa H, Takada K, Muranishi S
J Pharmacobiodyn. 1984 Jan;7(1):1-6. doi: 10.1248/bpb1978.7.1.
The permselectivity to the small intestinal blood-lymph barrier for the exogenous macromolecules absorbed from the lumen was investigated using in situ rat closed loop experiment. We chose the fluorescein isothiocyanate-labelled dextran (FD) as macromolecule and lipid-surfactant mixed micelles as an absorption promoter. The mean molecular weights of FDs used were 10500, 17500, 39000 and 64200 (abbreviated: FD10 , 20, 40 and 70). The lymph/plasma ratios of FDs concentrations during 5 h post administration were 0.2-1.2 ( FD10 ), 0.4-1.3 ( FD20 ), 1.3-7.2 ( FD40 ) and 2.6-11.9 ( FD70 ), respectively. The FD40 and FD70 levels in the lymph were significantly higher than those in the plasma. The cumulative amounts (% of the absorbed quantity) of FDs in the lymph from the lumen of the small intestine for 5 h after administration were 0.46% ( FD10 ), 0.51% ( FD20 ), 1.17% ( FD40 ) and 1.89% ( FD70 ), respectively. These findings suggest that the threshold molecular weight of FD for the transfer into the lymphatics with higher level compared to the blood concentration from the lumen across the small intestinal blood-lymph barrier exists between 17500 and 39000.
采用大鼠原位闭环实验,研究了从肠腔吸收的外源性大分子物质对小肠血 - 淋巴屏障的通透选择性。我们选择异硫氰酸荧光素标记的葡聚糖(FD)作为大分子物质,脂质 - 表面活性剂混合胶束作为吸收促进剂。所用FD的平均分子量分别为10500、17500、39000和64200(缩写:FD10、20、40和70)。给药后5小时内,FD浓度的淋巴/血浆比值分别为0.2 - 1.2(FD10)、0.4 - 1.3(FD20)、1.3 - 7.2(FD40)和2.6 - 11.9(FD70)。淋巴中FD40和FD70的水平显著高于血浆中的水平。给药后5小时内,从小肠肠腔进入淋巴的FD累积量(占吸收量的百分比)分别为0.46%(FD10)、0.51%(FD20)、1.17%(FD40)和1.89%(FD70)。这些发现表明,从小肠血 - 淋巴屏障跨膜进入淋巴且淋巴浓度高于血浓度的FD的阈值分子量介于17500和39000之间。